Sildenafil

別名:Revatio, UK-92480, Viagra

Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.

Sildenafil化学構造

CAS No. 139755-83-2

サイズ 価格(税別) 在庫状況
JPY 18100 国内在庫あり
JPY 51300 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(20)

カスタマーフィードバック1个实验数据

製品安全説明書

現在のバッチを見る: 純度: 99.97%
99.97

Sildenafil関連製品

シグナル伝達経路

PDE阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
human erythrocytes Function assay 60 mins Inhibition of ABCC5 in human erythrocytes assessed as inhibition of ATP-mediated [3H]cGMP uptake in inside-out vesicles after 60 mins by liquid scintillation counting, Ki=1.2 μM 22380603
HEK293T Function assay 2 hrs Displacement of [3H]ZM241385 from human AA2AR expressed in HEK293T cells after 2 hrs by liquid scintillation counter, Ki=0.19953μM 22563707
HEK293T Function assay 45 mins Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis, IC50=4.5μM 23122865
BL21-CodonPlus(DE3) Function assay 30 mins Inhibition of human His-tagged PDE5A catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method, IC50=0.0022μM 26908025
Sf9 Function assay 15 mins Inhibition of recombinant human PDE5A1 catalytic domain (535 to 860 residues) expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate incubated for 15 mins by liquid scintillation counting method, IC50=0.0022μM 26908025
BL21-CodonPlus(DE3) Function assay 30 mins Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method, IC50=20μM 26908025
Sf9 Function assay 30 mins Inhibition of full length recombinant human N-terminal GST-tagged PDE5A1 expressed in baculovirus infected Sf9 cells using cGMP as substrate after 30 mins by HTRF assay, IC50=0.004μM 27606546
Sf9 Function assay 1 hr Inhibition of N-terminal GST-tagged full length recombinant human PDE5A1 catalytic domain expressed in Baculovirus infected Sf9 insect cells using FAM-cGMP as substrate after 1 hr by fluorescence polarization assay, IC50=0.00365μM 29505934
Sf9 Function assay 30 mins Inhibition of N-terminal GST-tagged human PDE5A1 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay, IC50=0.00431μM 31021628
Sf9 Function assay 30 mins Inhibition of N-terminal GST-tagged human PDE6C expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay, IC50=0.03642μM 31021628
Sf9 Function assay 30 mins Inhibition of N-terminal GST-tagged human PDE1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay, IC50=0.819μM 31021628
Sf9 Function assay 30 mins Inhibition of N-terminal GST-tagged human PDE11A4 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay, IC50=4.93μM 31021628
RFL-6 Function assay Inhibition of phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells, Ki=0.0018μM 15771456
mammalian cells Function assay Inhibition of human Potassium channel HERG expressed in mammalian cells, IC50=3.31131μM 12873512
HEK293 Function assay TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells, IC50=20μM 12695538
CHO Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=3.31131μM 18448342
COS7 Function assay Inhibition of human recombinant PDE5A1 expressed in COS7 cells, IC50=0.075μM 18778098
Sf9 Function assay Inhibition of human PDE5A1 expressed in baculovirus in sf9 cells by PDE Glo phosphodiesterase assay, IC50=0.0056μM 25801159
BL21-CodonPlus Function assay Inhibition of recombinant human His6-tagged PDE5A (535 to 786 residues)/PDE6C expressed in Escherichia coli BL21-CodonPlus cells using [3H]cGMP as substrate, Ki=0.025μM 26908025
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
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生物活性

製品説明 Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.
Targets
PDE5 [1]
5.22 nM
In Vitro
In vitro Sildenafil improves insulin signalling and NO production in endothelial cells, probably by reducing oxidative stress induced by hyperglycemia and by increasing intracellular Ca2+ levels[2].
細胞実験 細胞株 HUVEC and HAEC
濃度 1 μM
反応時間 5 or 72 h
実験の流れ

HUVEC and HAEC from passages 3 to 6 are cultured for 72 hours in presence of 5.5 mmol/L glucose, 30 mmol/L glucose (high glucose; HG), 10 mmol/L Gluc-N with or without 1 µM of sildenafil (5 or 72 h) and/or 10−7 M insulin.

In Vivo
In Vivo Acute administration of the PDE-5 inhibitor sildenafil in a single clinically relevant dose does not modulate the in vivo function of the hypertrophic failing right heart of the rat measured by echocardiography and invasive hemodynamics[1].
動物実験 動物モデル Wistar rats
投与量 1 mg/kg
投与経路 i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05466695 Not yet recruiting
Erectile Dysfunction and Neutrophil Lymphocyte Ratio
Assiut University
August 1 2022 Early Phase 1
NCT05275725 Recruiting
Birth Asphyxia
Pia Wintermark|Kawempe National Referral Hospital|Saint Francis Memorial Hospital|Walimu|McGill University Health Centre/Research Institute of the McGill University Health Centre
July 1 2022 Phase 1
NCT04565925 Recruiting
Spinal Cord Injuries|Urinary Incontinence
The University of Texas Medical Branch Galveston
July 7 2021 Phase 2
NCT04122105 Unknown status
Renal Transplant Failure
University of British Columbia
April 1 2021 Not Applicable

化学情報

分子量 474.58 化学式

C22H30N6O4S

CAS No. 139755-83-2 SDF Download Sildenafil SDFをダウンロードする
Smiles CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C
保管

In vitro
Batch:

Water : 14 mg/mL

DMSO : Insoluble ( 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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